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401.
Synthesis and characterization of tributyltin derivatives from 4‐oxo‐4‐(arylamino)butanoic acids and their in vitro biological activity against cervical cancer cell lines 下载免费PDF全文
Irma Rojas‐Oviedo Carlos Camacho‐Camacho Luis Sánchez‐Sánchez Jorge Cárdenas Hugo López‐Muñoz Hugo Eugenio‐Robledo Israel Velázquez Rubén Alfredo Toscano 《应用有机金属化学》2014,28(12):884-891
Uterine (cervix and corpus) cancer is one of the major causes of mortality in women in Mexico. Organotin carboxylated derivatives have shown high cytotoxic activity against various cell lines of human origin. We describe the synthesis of three new tri‐n‐butyltin derivatives from 4‐oxo‐4‐(arylamino)butanoic acids; their structures were confirmed using spectral data (1H NMR, 13C NMR, 119Sn NMR and infrared), elemental analyses, mass spectrometry and X‐ray diffraction. All the tri‐n‐butyltin carboxylates exhibit 1 J (119/117Sn–13C) coupling satellites in solution and lie in the range 357 to 339 Hz, suggesting a tetrahedral geometry around the tin atom. The polymeric structures of two of the derivatives and the monomeric structure of another were confirmed using X‐ray crystallography. Using succinic anhydride as raw material, five N‐substituted succinamic acid compounds were synthesized by the acylation reaction with aniline, 4‐nitroaniline, 4‐nitro‐3‐(trifluoromethyl)aniline, 2‐amino‐5‐nitrothiazole and 4‐aminoantipyrine. From these compounds, five tin derivatives were prepared and their in vitro anti‐proliferative effect on HeLa, CaSki and ViBo cell lines was screened. All of the compounds showed potency against all three strains and null or low cytotoxic activity (necrotic) as well. The most potent of our derivatives as an anti‐proliferative agent against the three cell lines was tributylstannyl 4‐oxo‐4‐[(3‐trifluoromethyl‐4‐nitrophen‐1‐yl)amino]butanoate, exhibiting an IC50 value of 0.43 μM against the HeLa cell line. Copyright © 2014 John Wiley & Sons, Ltd. 相似文献
402.
Rubn Toscano Mnica Moya Carlos Amabile Guillermo Penieres Cecilio Alvarez 《Heteroatom Chemistry》2000,11(4):308-312
The synthesis, characterization and biological activity of N′‐trifluoromethanesulfonyl‐2‐aminopyridine in connection with our studies of trifluoromethanesulfonyl derivatives of the pyridine ring have been achieved. In solution an equilibrium (∼ 50:50%) of the amide and imide tautomeric forms was observed, while in the solid state only the imide form was present. Biological tests on the compound showed no effect either upon the growth of Escherichia coli or on Staphylococcus aureus in the agar diffusion tests; however, the growth of Enterococcus faecalis was effectively inhibited. © 2000 John Wiley & Sons, Inc. Heteroatom Chem 11:308–312, 2000 相似文献